ARRY-380 Inhibitor CAS No. 937265-83-3

Cat. No.	Name	Size	Price
KI2826	ARRY-380	5 mg	$432
	ARRY-380	10 mg	$592
	ARRY-380	20 mg	$946
	ARRY-380	50 mg	$1712
	ARRY-380	100 mg	$2738
	ARRY-380	200 mg	$3952
	ARRY-380	1 g	$10116

Chemical Characteristic

Product Name	ARRY-380
CAS No.	937265-83-3
Molecular Weight	569.63
Formula	C₂₉H₂₇N₇O₄
Chemical Name	6-[5-[(2-methylsulfonylethylamino)methyl]furan-2-yl]-N-[3-methyl-4-([1,2,4]triazolo[1,5-a]pyridin-7-yloxy)phenyl]quinazolin-4-amine
Smiles	n1cnc(c2cc(ccc12)c1oc(cc1)CNCCS(=O)(=O)C)Nc1cc(c(cc1)Oc1cc2n(cc1)ncn2)C
Chemical Structure

Biological activities

ARRY-380 is a potent and selective HER2 (also known as ErbB2) inhibitor. The IC50 values of ARRY-380 against HER2 and truncated p95-HER2 are 8 and 7 nM, respectively.^[1] ARRY-380 administration (25-100 mg/kg) produces dose-related inhibition of BT474 tumor growth. ARRY-380, at of 100 mg/kg does, has a maximum inhibition (81%). Moreover, ARRY-380 significantly inhibits BT-474 tumor growth at 50 and 100 mg/kg. ARRY-380 at 50 mg/kg, in combination with bevacizumab, shows significantly enhanced activity compared to either agent alone in SK-OV-3 tumor xenograft model.^[2]

References

[1] Moulder S L, et al. ARRY-380, a selective HER2 inhibitor: From drug design to clinical evaluation. Molecular Cancer Therapeutics. 2011, 10 (11): A143 [2] Patrice Lee, et al. In Vivo Activity of ARRY-380, a Potent, Small Molecule Inhibitor of ErbB2 in Combination with Trastuzumab, Docetaxel or Bevacizumab. Nihon Yakurigaku Zasshi.

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